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Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist.
Betahistine (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) with acute administration has increased tele-methylhistamine (t-MeHA) levels with an ED50 of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED50 of 2 mg/kg in male Swissmice. Betahistine (oral adminstration; 1 and 5 mg/kg; daily for 3 weeks) attenuates the severity of arthritis and reduces the levels of pro-inflammatory cytokines in the paw tissues of CIA mice.
| Molecular Weight | 136.19 |
| Formula | C8H12N2 |
| CAS Number | 5638-76-6 |
| Form | Liquid (density 0.984 g/mL) |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage | 4°C, dry, sealed |
[4] Louisa Murdin, et al. Cochrane Database Syst Rev. Betahistine for symptoms of vertigo
| Related Histamine Receptor Products |
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| Ciproxifan maleate
Ciproxifan is an orally bioavailable, extremely potent histamine H3 inverse agonist/antagonist. |
| Antazoline hydrochloride
Antazoline hydrochloride is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. |
| Azacyclonol
Azacyclonol, also known as γ-pipradol, which diminishes hallucinations in psychotic individuals. |
| Azatadine dimaleate
Azatadine dimaleate is an antihistamine and anticholinergic compound with IC50 of 6.5nM and 10nM, respectively. |
| Bepotastine Besilate
Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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